Preparation of CI-921 mixed micelles and determination of its entrapment efficiency by method of dialysis and fitting
10.11665/j.issn.1000-5048.20160512
- VernacularTitle:CI-921混合胶束的制备及透析拟合法测定胶束的包封率
- Author:
Weisai ZHOU
1
;
Zimei WU
;
Bruce C BAGULEY
;
Caibin LI
;
Wenli ZHANG
;
Jianping LIU
Author Information
1. 中国药科大学药剂学教研室
- Publication Type:Journal Article
- Keywords:
CI-921;
Pluronic F127;
Solutol HS15;
mixed micelles;
method of dialysis and fitting;
entrapment efficiency
- From:
Journal of China Pharmaceutical University
2016;47(5):575-580
- CountryChina
- Language:Chinese
-
Abstract:
The aim of this research were to prepare CI-921 mixed micelles(CI-Micelles), to establish a method for determining the entrapment efficiency of CI-Micelles, to optimize the formulation and to evaluate their in vitro properties. CI-Micelles were prepared by film dispersion. Dialysis and fitting were used to calculate true entrapment efficiency(EE)and drug loading(DL)of CI-Micelles. The influences of polymer concentration, polymer radio and hydrating media on the entrapment efficiency, drug loading and particle-size were investigated. The stability at 4 °C in 6 days was evaluated. The optimal formulation of CI-921-Micelles consisting of polymer concentration of 72 mg/mL, a mass radio of Pluronic F127/Solutol HS15 at mass ratio of 1 ∶2 and 5% glucose solution as hydrating medium, showed a EE of more than 90%, and mean particle-size of 17-25 nm and PDI< 0. 210. There were no significant changes to CI-Micelles in EE and particle-size after treatment at 4 °C for 6 days. The applied method of dialysis and fitting could be used to determine EE for micelles loaded with weakly basic drug which was difficult to meet sink conditions. Adjustment of the mass radio of Pluronic F127 to Solutol HS15 had resulted in uniform particle size distribution, high entrapment efficiency and drug loading capacity and better stability of CI-Micelles.
